Varenicline (CP 526555) dihydrochloride is a potent partial agonist forα4β2 nicotinic acetylcholine receptor (nAChR)with anEC₅₀value of 2.3 μM. Varenicline dihydrochloride is a full agonist for α3β4 and α7 nAChRs withEC₅₀values of 55 μM and 18 μM, respectively^[2]. Varenicline dihydrochloride is a nicotinic ligand based on the structure of cytosine, and has the potential for smoking cessation treatment^[5].

EC50: 2.3 μM (α4β2 nAChR); 18 μM (α7 nAChR); 55 μM (α3β4 nAChR)^[2]

Varenicline dihydrochloride (1 μM, 24 h ) inhibits LPS-Induced cytokine secretions (IL-1β, IL-6, and TNF_α) and cell proliferation rate in RAW 264.7 macrophages^[1].
Varenicline dihydrochloride (250 nM) evokes action potentials (Aps) in the absence of ACh stimulation in Human adrenal chromaffin cells isolated from male and female organ donors^[3].
Varenicline dihydrochloride (100 μM, 4 h) promotes migration of HUVECs by lowering the protein expression of VE-cadherin^[4].

Varenicline dihydrochloride (Subcutaneous injection, 0.01-1 mg/kg, 3 days) given 10 min prior to nicotine (0.5 mg/kg, s.c.) inhibits nicotine conditioned place preference (CPP)^[5].
Varenicline dihydrochloride (Subcutaneous injection, 2.5 mg/kg, 3 days) results in a place aversion which is dependent on α5 nAChRs but not β2 nAChRs^[5].
Varenicline dihydrochloride (Subcutaneous injection, 0.1 and 0.5 mg/kg, 3 days) reverses nicotine withdrawal signs such as hyperalgesia and somatic signs and withdrawal-induced aversion in a dose-related manner^[5].

284.18

C₁₃H₁₅Cl₂N₃

866823-63-4

伐尼克兰二盐酸盐

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.